ES2305452T3 - Inhibidores de la catepsina cisteina y proteasa. - Google Patents

Inhibidores de la catepsina cisteina y proteasa. Download PDF

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Publication number
ES2305452T3
ES2305452T3 ES03716238T ES03716238T ES2305452T3 ES 2305452 T3 ES2305452 T3 ES 2305452T3 ES 03716238 T ES03716238 T ES 03716238T ES 03716238 T ES03716238 T ES 03716238T ES 2305452 T3 ES2305452 T3 ES 2305452T3
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Spain
Prior art keywords
alkyl
optionally substituted
heterocyclyl
alkenyl
so2r
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Expired - Lifetime
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ES03716238T
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English (en)
Inventor
Christopher I. Bayly
Cameron Black
Serge Leger
Chun Sing Li
Dan Mckay
Christophe Mellon
Jacques Yves Gauthier
Cheuk Lau
Michel Therien
Vouy-Linh Truong
Michael J. Green
Bernard L. Hirschbein
James W. Janc
James T. Palmer
Chitra Baskaran
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Merck Canada Inc
Axys Pharmaceuticals Inc
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Merck Frosst Canada Ltd
Axys Pharmaceuticals Inc
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    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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Abstract

La presente invención se refiere un compuestos de la siguiente fórmula química: (Ver fórmula) en la que R 1 es hidrógeno, alquilo C1 - 6 o alquenilo C2 - 6 en la que dichos grupos alquilo y alquenilo están opcionalmente sustituidos con uno a seis halógenos, cicloalquilo C3 - 6, -SR 9 , -SR 12 , -SOR 9 , -SOR 12 , -SO2R 9 , -SO2R 12 , -SO2CH (R 12 )(R 11 ), -OR 12 , -OR 9 , -N(R 12 )2, arilo, heteroarilo o heterociclilo en la que dichos grupos arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o dos sustituyentes seleccionados independientemente de alquilo C1 - 6, halógeno, hidroxialquilo, hidroxilo, alcoxilo o ceto; R 2 es hidrógeno, alquilo C1 - 6 o alquenilo C2 - 6 en la que dichos grupos alquilo y alquenilo están opcionalmente sustituidos con uno a seis halógenos, cicloalquilo C3 - 6, -SR 9 , -SR 12 , -SOR 9 , -SOR 12 , -SO2R 9 , -SO2R 12 , -SO2CH(R 12 )(R 11 ), -OR 12 , -OR 9 , -N(R 12 )2, arilo, heteroarilo o heterociclilo en la que dichos grupos arilo, heteroarilo y heterociclilo están opcionalmente sustituidos con uno o dos sustituyentes seleccionados independientemente de alquilo C1 - 6, halógeno, hidroxialquilo, hidroxilo, alcoxilo o ceto; o R 1 y R 2 pueden tomarse junto con el átomo de carbono al que están unidos para formar un anillo de heterociclilo o cicloalquilo C3 - 8 en la que dicho sistema de anillo está opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente de alquilo C1 - 6, hidroxialquilo, haloalquilo o halógeno; R 3 es hidrógeno, alquilo C1 - 6 o alquenilo C2 - 6 en la que dichos grupos alquilo y alquenilo están opcionalmente sustituidos con cicloalquilo C3 - 6 o uno a seis halógenos; R 4 es...
ES03716238T 2002-03-05 2003-02-28 Inhibidores de la catepsina cisteina y proteasa. Expired - Lifetime ES2305452T3 (es)

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